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CE3F4

Catalog No. T12616L CAS 143703-25-7

CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1; IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively).

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CE3F4, CAS 143703-25-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 80.00
25 mg	In stock	$ 156.00
50 mg	In stock	$ 288.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 97.15%

Purity: 98%

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Description	CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1; IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively).
Targets&IC50	Epac1:10.7 μM, Epac2B:66 μM
In vitro	CE3F4 is a selective antagonist of Epac1, with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively. CE3F4 is more active on Epac1 than (S)-stereoisomer ((S)-CE3F4, IC50, 56 μM), but less active than (R)-CE3F4 (IC50, 5.8 μM). CE3F4 (20 μM) inhibits Epac-induced Rap1 activation in living cultured HEK293 cells[2] and CE3F4 (20 μM) significantly inhibits the late phase of ERK activation stimulated by glucose in INS-1 cells[3]. CE3F4 (40 μM) specifically inhibits Epac1 guanine nucleotide exchange activity without interference with Rap1 activity or Epac1-Rap1 interaction. CE3F4 (50 μM) shows more inhibitory activities against GEF activity of Epac1, than that of Epac2(AB) or Epac2(B)[1]. CE3F4 reduces the exchange activity of Epac1 induced by 007, with IC50 of 23 ± 3 μM. CE3F4 has no influence on PKA activity.

Molecular Weight	351.01
Formula	C11H10Br2FNO
CAS No.	143703-25-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (142.45 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Courilleau D, et al. The (R)-enantiomer of CE3F4 is a preferential inhibitor of human exchange protein directly activated by cyclic AMP isoform 1 (Epac1). Biochem Biophys Res Commun. 2013 Oct 25;440(3):443-8. 2. Courilleau D, et al. Identification of a tetrahydroquinoline analog as a pharmacological inhibitor of the cAMP-binding protein Epac. J Biol Chem. 2012 Dec 28;287(53):44192-202. 3. Pratt EP, et al. Ca2+ influx through L-type Ca2+ channels and Ca2+-induced Ca2+ release regulate cAMP accumulation and Epac1-dependent ERK 1/2 activation in INS-1 cells. Mol Cell Endocrinol. 2016 Jan 5;419:60-71.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Bioactive Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Inhibitor Library

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Keywords

CE3F4 143703-25-7 GPCR/G Protein cAMP inhibit Inhibitor CE-3F4 inhibitor

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